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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，1 year;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，1 year;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
PZ-128
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
371131-16-7
- 规格：
25mg/10mg/5mg
| 规格： | 25mg | 产品价格： | ￥4990.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥2490.0 |
| 规格： | 5mg | 产品价格： | ￥1490.0 |
| 基本信息 | |
| CAS | No.371131-16-7 |
| 英文名称 | PZ-128 |
| 分子式 | C55H99N13O9 |
| 分子量 | 1086.46 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:-20℃，1 year;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD32874091 |
| SMILES | CCCCCCCCCCCCCCCC(=O)NC(CCCCN)C(=O)NC(CCCCN)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC(C)C(=O)NC(CC(C)C)C(=O)NC(CC1=CC=CC=C1)C(=O)N |
| InChIKey | VZRIKWNVDCTBTF-BKGFHLQYSA-N |
| InChI | InChI=1S/C55H99N13O9/c1-5-6-7-8-9-10-11-12-13-14-15-16-20-31-47(70)63-41(28-21-23-32-56)51(74)64-42(29-22-24-33-57)52(75)68-46(37-69)54(77)65-43(30-25-34-61-55(59)60)50(73)62-39(4)49(72)67-45(35-38(2)3)53(76)66-44(48(58)71)36-40-26-18-17-19-27-40/h17-19，26-27，38-39，41-46，69H，5-16，20-25，28-37，56-57H2，1-4H3，(H2，58，71)(H，62，73)(H，63，70)(H，64，74)(H，65，77)(H，66，76)(H，67，72)(H，68，75)(H4，59，60，61)/t39-，41-，42-，43-，44-，45-，46-/m0/s1 |
| PubChem CID | 72187679 |
| 靶点 | PAR1 |
| 通路 | GPCR & G Protein |
| 背景说明 | PZ-128是一种特异性的且可逆的PAR1拮抗剂。PZ-128 具有抗血小板，抗转移，抗血管生成和抗癌活性。 |
| 生物活性 | PZ-128 (P1pal-7)， a cell-penetrating lipopeptide pepducin， is a first-in-class， specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet， anti-metastatic， anti-angiogenic and anticancer effects[1][2][3][4]. |
| In Vitro | PZ-128 (P1pal-7; 3 μM) blocks 90-94% of OVCAR-4 migration toward human ovarian ascites and fibroblast conditioned media. The OVCAR4-treated peritoneal fibroblast conditioned media elicits a 2.2-fold increase in endothelial barrier permeability which could be nearly completely inhibited by PZ-128[1].PZ-128 is a lipidated ‘pepducin which targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G proteins. The structure of PZ-128 is found to mimic the off-state of the corresponding intracellular region of PAR1 which is critical for coupling to G proteins[3]. |
| 细胞实验 | PZ-128 (P1pal-7; 10 mg/kg; intraperitoneal injection; every other day; for 6 weeks) treatment significantly reduces mean ascites fluid volume by 60%. PZ-128 treatment also causes a highly significant 84-96% reduction in blood vessel density in both the center and edge of the OVCAR-4 tumors[1].Animal Model: Female NCR Nu/Nu mice (5-7 weeks) injected with OVCAR-4 or SKOV-3 cells[1]；Dosage:10 mg/kg；Administration:Intraperitoneal injection; every other day; for 6 weeks；Result: Significantly reduced mean ascites fluid volume by 60%. |
| 数据来源文献 | [1]. Anika Agarwal， et al. Targeting a metalloprotease-PAR1 signaling system with cell-penetrating pepducins inhibits angiogenesis， ascites， and progression of ovarian cancer. Mol Cancer Ther. 2008 Sep;7(9):2746-57. [2]. Lidija Covic， et al. Protease-Activated Receptor 1 as Therapeutic Target in Breast， Lung， and Ovarian Cancer: Pepducin Approach. Int J Mol Sci. 2018 Jul 31;19(8):2237. [3]. Ping Zhang， et al. Suppression of arterial thrombosis without affecting hemostatic parameters with a cell-penetrating PAR1 pepducin. Circulation. 2012 Jul 3;126(1):83-91. [4]. Paul A Gurbel， et al. Cell-Penetrating Pepducin Therapy Targeting PAR1 in Subjects With Coronary Artery Disease. Arterioscler Thromb Vasc Biol. 2016 Jan;36(1):189-97. |
| 单位 | 瓶 |
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文献和实验_ChIP_method.html Chromatin IP Method, ChIP buffers, Notes on ChIP Method, Quantative PCR using 32P dCTP. Hahn Lab. ChIP Assay Protocol PDF - /attach/2008/2008-02-01/2B/2B6C4EA25F257424710A50E83CB2F380.pdf Formaldehyde cross-linking
5+YiLLj4HREBXstjztk7uH3PDncf2sPhxRlMq6wGF+vZ2OlE8VGoBH85gWn/XYBn2ck48eAqDu+xwjbrU7h2Zz2aZ3fD6YWWeBFuzJv2yfAMMyYBFj4y5r7yqpgAE0jPBFRyolzbpihAeo1X9z5K2o2YlqOUxRTN25rQLQ+8+x4oVfFzvgFHklZM2raEadaIsxjVfI0wedUizB5fB7r8yR8TTr6mQAL8FlQgbB6KCTABJiAfgWD8ev0cIrh
Peak在TSS上下游的分布图是ChIP测序中非常关键的一张图。有这张图，我们就能知道目的蛋白（组蛋白或转录因子）在转录起始位点（TSS）及上下游附近的整体分布/结合情况。 图中横坐标为基因位置，纵坐标为reads的覆盖深度，它可以反映目的蛋白分布情况。input由于没有富集，其reads通常分布较低，而IP对目的蛋白及其结合序列的富集作用则会使reads覆盖深度提高，产生相应的结合峰。TSS上下游通常是组蛋白和转录因子主要结合、调控的区域，所以也是大量出现结合峰的区域
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